Ulixertinib (BVD-523, VRT752271)

Catalog No.S7854

Molecular Weight(MW): 433.33

Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.

Cited by 1 Publication

Int J Clin Exp Med, 2016, 9(6):10955-10962

PubMed:

1 Customer Review

Ulixertinib inhibited the proliferation of SUDHL-10 and Raji cells. (A) The activation of ERK1/2 was analyzed by Western blotting. Ulixertinib (0.1, 0.4 and 1.0 nM) significantly inhibited ERK1/2 activation in a dose-dependent manner compared with control cells. Cell proliferation was measured by the CCK-8 assay. Ulixertinib (0.1, 0.4 and 1.0 nM) significantly inhibited proliferation of SUDHL-10 (B) and Raji cells (C) in a time- and dose-dependent manner compared with control cells.

Int J Clin Exp Med, 2016, 9(6):10955-10962.. Ulixertinib (BVD-523, VRT752271) purchased from Selleck.

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Choose Selective ERK Inhibitors

Biological Activity

Description

Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.

Targets

ERK1 ^[1]	ERK2 ^[1]
	<0.3 nM

In vitro

In an A375 melanoma cell line containing a b-RAFV600E mutation, Ulixertinib reduces the levels of phosphorylated ERK2 (pERK) and of the phosphorylation of the downstream kinase RSK (pRSK) with IC50 of 4.1/0.14 μM, respectively. Ulixertinib also inhibits A375 cell proliferation with IC50 of 180 nM. ^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
human A375 cells	MX7GeY5kfGmxbjDhd5NigQ>?		NF7UbmwzKGh?		MYrJcohq[mm2aX;uJI9nKEWUS{GvNkBqdiCqdX3hckBCOzd3IHPlcIx{KGijcnLvdolv\yCELWLBSkBXPjByRTDteZRidnRiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4heGixc4Doc{1TW0tibHX2[Ywh[W[2ZYKgNkBpenNiYomgR4VtdG:vaXPzJGFzemG7U3PhcnROKF[WSTDpcYFocW6pIHHuZYx6e2m\|LDDJR\|UxRTBwMUSg{txO	MYGyOVk4Pzl6MR?=
human A375 cells	Mle4VJJwdGmoZYLheIlwdiCjc4PhfS=>		M1e0c\|czKGh?		MWDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF\|N{WgZ4VtdHNiaHHyZo9zcW6pIFKtVmFHKFZ4MEDFJI12fGGwdDDh[pRmeiB5MjDodpMh[nliQ3XscI9ucWO\|IFHydoF6W2OjbmTNJHZVUSCrbXHnbY5oKGGwYXz5d4l{NCCLQ{WwQVAvOThizszN	M2P2RlI2QTd5OUix

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:^[1]	+ Expand ERK2 Rapidfire Mass Spectrometry Inhibition of Catalysis Assay: MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are made up in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl₂, 0.1 mM EGTA, 10 mM DTT and 0.01% (v/v) CHAPS. 1.2 nM ERK2 protein is prepared in assay buffer and 10 µL is dispensed into each well of a polypropylene, 384-well plate containing test and reference control compounds. The compound plates had previously been dosed with a 12 point range from 100 µM down to 0.1 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 20 minute pre-incubation of enzyme and compound at room temperature, 10 µL of substrate solution is added consisting of 16 µM Erktide (IPTTPITTTYFFFK) and 120 µM ATP (measured Km) in assay buffer. The reaction is allowed to progress for 20 minutes at room temperature before being quenched by the addition of 80 µl 1% (v/v) formic acid. The assay plates are then run on the RapidFire Mass Spectrometry platform to measure substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels.
Cell Research:^[1]	+ Expand Cell lines: A375 cells Concentrations: ~30 μM Incubation Time: 72 h Method: A375 cells are cultured in cell media composed of DMEM, 10% (v/v) Foetal Calf Serum and 1% (v/v) L-Glutamine. After harvesting, cells are dispensed into black, 384-well Costar plates to give 200 cells per well in a total volume of 40 µL cell media, and are incubated overnight at 37°C, 90% relative humidity and 5% CO₂ in a rotating incubator. Test compounds and reference controls are dosed directly into the cell plates, into the inner 308 wells, using a Labcyte Echo 555 acoustic dispenser. The cells are dosed over a 12 point range from 30 µM down to 0.03 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 0.3%. The cell plates are then incubated for 72 hours at 37°C. Cells were fixed and stained by the addition of 20 µL 12% formaldehyde in PBS/A (4% final concentration) and 1:2000 dilution of Hoechst 33342, with a 30 minute room temperature incubation, and then washed with PBS/A. A cell count is performed on the stained cell plates using a Cellomics ArrayScanTM VTI imaging platform. A Day 0 cell plate is also fixed, stained and read to generate a cell count baseline for determining compound cytotoxic effects as well as anti-proliferative effects. (Only for Reference)

Kinase Assay:^[1]

+ Expand

ERK2 Rapidfire Mass Spectrometry Inhibition of Catalysis Assay:

MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are made up in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl₂, 0.1 mM EGTA, 10 mM DTT and 0.01% (v/v) CHAPS. 1.2 nM ERK2 protein is prepared in assay buffer and 10 µL is dispensed into each well of a polypropylene, 384-well plate containing test and reference control compounds. The compound plates had previously been dosed with a 12 point range from 100 µM down to 0.1 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 20 minute pre-incubation of enzyme and compound at room temperature, 10 µL of substrate solution is added consisting of 16 µM Erktide (IPTTPITTTYFFFK) and 120 µM ATP (measured Km) in assay buffer. The reaction is allowed to progress for 20 minutes at room temperature before being quenched by the addition of 80 µl 1% (v/v) formic acid. The assay plates are then run on the RapidFire Mass Spectrometry platform to measure substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels.

Cell Research:^[1]

+ Expand

Cell lines: A375 cells
Concentrations: ~30 μM
Incubation Time: 72 h
Method: A375 cells are cultured in cell media composed of DMEM, 10% (v/v) Foetal Calf Serum and 1% (v/v) L-Glutamine. After harvesting, cells are dispensed into black, 384-well Costar plates to give 200 cells per well in a total volume of 40 µL cell media, and are incubated overnight at 37°C, 90% relative humidity and 5% CO₂ in a rotating incubator. Test compounds and reference controls are dosed directly into the cell plates, into the inner 308 wells, using a Labcyte Echo 555 acoustic dispenser. The cells are dosed over a 12 point range from 30 µM down to 0.03 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 0.3%. The cell plates are then incubated for 72 hours at 37°C. Cells were fixed and stained by the addition of 20 µL 12% formaldehyde in PBS/A (4% final concentration) and 1:2000 dilution of Hoechst 33342, with a 30 minute room temperature incubation, and then washed with PBS/A. A cell count is performed on the stained cell plates using a Cellomics ArrayScanTM VTI imaging platform. A Day 0 cell plate is also fixed, stained and read to generate a cell count baseline for determining compound cytotoxic effects as well as anti-proliferative effects.
(Only for Reference)

References

[1] Ward RA, et al. J Med Chem. 2015, 58(11), 4790-4801.

Solubility (25°C)

In vitro	DMSO	86 mg/mL (198.46 mM)
	Ethanol	15 mg/mL (34.61 mM)
	Water	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Ulixertinib (BVD-523, VRT752271) SDF

Molecular Weight	433.33
Formula	C₂₁H₂₂Cl₂N₄O₂
CAS No.	869886-67-9
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2018-10-19)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02608229	Recruiting	Pancreatic Cancer\|Cancer of Pancreas\|Cancer of the Pancreas\|Pancreas Cancer	Washington University School of Medicine\|BioMed Valley Discoveries Inc\|National Cancer Institute (NCI)	June 6 2016	Phase 1
NCT03454035	Recruiting	Tumor Solid\|Pancreatic Cancer	UNC Lineberger Comprehensive Cancer Center\|BioMed Valley Discoveries Inc\|Pfizer	January 30 2018	Phase 1
NCT03417739	Recruiting	Uveal Melanoma	Dana-Farber Cancer Institute\|BioMed Valley Discoveries Inc	March 26 2018	Phase 2
NCT02994732	Completed	Healthy	BioMed Valley Discoveries Inc	January 2017	Phase 1
NCT02296242	Completed	Acute Myelogenous Leukemia\|Myelodysplastic Syndrome	BioMed Valley Discoveries Inc	November 2014	Phase 1\|Phase 2
NCT01781429	Completed	Advanced Solid Tumors	BioMed Valley Discoveries Inc	March 2013	Phase 1\|Phase 2

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Ulixertinib (BVD-523, VRT752271)

Cited by 1 Publication

1 Customer Review

Purity & Quality Control

Choose Selective ERK Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download Ulixertinib (BVD-523, VRT752271) SDF

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The Serial Dilution Calculator Equation

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2018-10-19)

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Ulixertinib (BVD-523, VRT752271)

Cited by 1 Publication

1 Customer Review

Purity & Quality Control

Choose Selective ERK Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download Ulixertinib (BVD-523, VRT752271) SDF

Bio Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Dilution Calculator

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

Instructions to calculate molar mass (molecular weight) of a chemical compound:

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2018-10-19)

Tech Support

ERK Signaling Pathway Map

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)